摘要
采用超声薄膜水化法制备包裹大豆异黄酮主要功能成分染料木黄酮(Ge)的甘露糖修饰聚乙二醇化纳米脂质体(manPEG@LP/Ge)。伴刀豆球蛋白A(ConA)凝集实验证实甘露糖能够成功修饰在纳米脂质体表面。manPEG@LP/Ge呈规则的球形,大小分布均一,颗粒分散性好。其粒径为(270±15) nm,Zeta电位为+7.5 mV。由于聚乙二醇(PEG)长链的空间位阻效应和颗粒所带正电荷的排斥作用实现了较强的结构刚性和较好的稳定性。流式细胞术的结果表明:manPEG@LP/Ge能够特异性的识别甘露糖受体高表达的人肝癌Huh7细胞。细胞毒理实验证明:药物载体manPEG@LP本身没有毒副作用,生物相容性较好。细胞水平和动物水平的肿瘤杀伤实验结果表明:运载药物之后的manPEG@LP/Ge在甘露糖介导的“主动靶向”作用下高效而特异性的进入肿瘤细胞,对肿瘤组织进行了有效地杀伤。
Abstract
Genistein doped mannoseconjugated PEGmodified liposomes (manPEG@LP/Ge) were prepared via filmsonic method by using targeted lipid DSPEPEGman and helper lipid DOTAP. Concanavalin A (ConA) agglutination assay had proved that mannose has been modified to nanoliposomes successfully. The asprepared manPEG@LP/Ge were spherical in shape with a homogeneous size distribution around (270±15) nm in diameter as characterized by SEM. The Zeta potential was +7.5 mV in pure water. Furthermore, manPEG@LP/Ge appeared to be very homogeneous and stable in water. It is considered that the sterichinerance effects of surface PEG long chain and the strong electrostatic repulsion of the positive charge play an important role in the good dispersion of manPEG@LP/Ge. Flow cytometry examination confirmed the targeting specificity of manPEG@LP/Ge against human hepatoma Huh7 cells which are of overexpression of mannose receptors. The cell toxicity viability demonstrated that unloaded manPEG@LP are practically nontoxic, indicating that the drug delivery vehicles possess excellent biocompatibility. Systematic in vitro and in vivo studies showed that the manPEG@LP/Ge kill tumor cells with high specificity and excellent efficiency, owing to the mannosemediated active tumortargeted drug delivery.
杨〓凡,秦爱平,李〓璟,彭〓倩,王晨旭,洪秀琴.
基于包裹染料木黄酮的甘露糖靶向长循环纳米脂质体抗肿瘤效应研究[J]. 激光生物学报. 2017, 26(4): 334-341
Targeting and Long Circulating Drug Delivery System Base on Mannoseconjugated PEGmodified Nanoliposomes for Tumor Chemotherapy[J]. Acta Laser Biology Sinica. 2017, 26(4): 334-341
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